克山病和大骨节病患者红细胞免疫功能与血硒水平的对比研究

对潜在型克山病和大骨节病患者的红细胞免疫功能、血清红细胞免疫粘附调节因子和全血硒含量进行了检测。结果表明：克山病和大骨节病患者的红细胞Ｃ３ｂ受体花环率和全血硒含量均明显低于非病区居民，血清红细胞免疫粘附抑制率均高于非病区居民，免疫复合物花环率和血清红细胞免疫粘附促进率与非病区居民无明显差异；但两病患者上述参数之间无明显差异。提示潜在型克山病和大骨节病患者红细胞免疫功能低下，可能均与低硒状态和血清红     

低硒克山病病区和非病区居民红细胞免疫功能的对比测定

对比测定了低硒克山病病区和非病区居民的红细胞免疫功能、血清红细胞免疫粘附调节因子和血硒含量。结果表明，低硒病区和非病区居民红细胞Ｃ３ｂＲ花环率和血硒水平显著低于对照非病区，而血清红细胞免疫粘附花环抑制率显著高于对照非病区；３组居民的红细胞免疫复合物花环率和血清红细胞免疫粘附花环促进率无明显差异；低硒病区和非病区居民上述各参数值均相似。研究说明，克山病病区居民红细胞免疫功能低下和血清红细胞免疫粘附抑     

陕西省克山病病区儿童和成人发锰含量测定

用原子吸收光谱法测定了陕西省彬县克山病房区克山病房户、非病户和非病区礼泉县对照户儿童和成人发锰含量．结果表明。1．病户儿童发锰明显高于非病区对照户，病区非病户儿童与病户或非病区对照户无明显差异；2．3组成人发锰差异不明显；3．病区病户和非病户儿童发锰均明显高于成人，非病区对照户儿童和成人发锰含量无显著差异．     

克山病病区硒水平监测的10年总结

对陕西省黄陵县克山病病工欠群内外环境硒水平进行了１０年动态监测。结果表明：①当地产小麦、大米、玉米和黄豆硒含量监测是无明显变化,均仍低于非病区同种粮食硒水平,病区居民所食外地麦面硒含量明显高于当地产小麦硒含量;②病区儿童发硒含量明显上升并已达到非病区水平;③病区人群内环境硒水平提高。可能与食用外地表现和硒磺盐有关。     

克山病病区和常硒及低硒非病区儿童发铜,锌,铁,锰含量的测定

用原子吸收光谱法测定了克山病病区,常硒非病硒非病区儿童区Ｃｕ、Ｚｎ、Ｆｅ、Ｍｎ含量,结果表明：（１）低硒非病区组儿童发Ｃｕ、Ｚｎ、Ｆｅ、Ｍｎ含量与常硒非病区组无明显差异。（２）克山病病区组儿童ｕ、Ｚｎ、Ｍｎ民低硒和常硒非病区组儿童无明显差异。     

克山病病情与人体硒水平的17年监测

１９７３￣１９９０年对陕西省黄陵县店头病区克山病消长与人体硒水平进行了动态观察。观察期间，急型（含急型和亚急型）、慢型和潜在型克山病发病率逐年下降，潜在型病情恶化率亦下降趋势；病区人群头发硒含量逐年上升，病情与发硒含量呈显著负相关。病区人群头发硒含量提高至非病区农村水平后，慢型和潜在型仍有新发病。     

大骨节病,克山病共存区及特异病区血硒及有关生化指标的测定

测定了陕西彬县大骨节病区、克山病存区，云南牟定单纯克山病区、陕西安康“高硒”大骨节病区及四川南部低硒无病区人血硒、维生素Ｃ及磷含量。结果表明，以低硒为中心的代谢紊乱是克山病、大骨节病区人群共同具有的基本生化特征，低硒仍是两病发病的重要因素；病区人群缺硒的同时伴有维生素Ｃ的缺乏或相对缺乏；大骨节病区人群低硒较克册病区人群更加明显，两病区儿童低硒较成人更加明显。     

补充富硒小麦和富硒玉米对大鼠血硒状态影响的对比观察

给克山病病区粮喂养６周的大鼠补充富硒小麦或富硒玉米,观察了大鼠血硒和血ＣＳＨ－Ｐｘ活性的变化。结果显示,补充富硒小麦和富硒玉米均可有效地升高大鼠血浆硒、红细胞硒和红细胞ＧＳＰ－Ｐｘ活性,且两种形式硒的作用效果相同;停止补硒后,补充富硒小麦组大鼠的红细胞和红细胞ＧＳＨ－Ｐｘ活性均显著高于补充富硒玉米组大鼠。表明给大鼠补充富硒小麦较补充富硒玉米好。     

河南省地甲病、克山病、大骨节病病区不同人群发硒含量及全血GSH-Px活性的对比分析

测定了河南省地甲病、克山病、大骨病病区不同人群发硒含量及GSH－Px活性，并作了对比分析，结果表明，对照组人群发硒含量及GSH－Px活力显著高于地甲病、克山病及大骨节病区，病区之间无显著性差异。     

河南省地方甲病,克山病,大骨节病病区不同人群发硒含量及全…

测定了河南省地甲病，克山病，大骨病病区不同人群发硒含量及ＧＳＨ－Ｐｘ活性，并作了对比分析，结果表明，对照组人群发硒含量及ＧＳＨ－Ｐｘ活力显著高于地甲病，克山病及大骨节病区，病区之间无显著性差异。     

α-Amino acid derived enaminones and their application in the synthesis of N-protected methyl 5-substituted-4-hydroxypyrrole-3-carboxylates and other heterocycles

A new and simple synthesis of novel N-protected methyl 5-substituted-4-hydroxypyrrole-3-carboxylates, which exist in equilibrium with their 4-oxo tautomers, has been developed in two steps starting from N-protected α-amino acids. The key intermediates are enaminones, which can also be isolated, characterized, and used for the construction of other functionalized heterocycles, before they spontaneously decompose to pyrrole products. 4-Hydroxypyrroles are prone to partial aerial oxidation but can be efficiently alkylated or reduced to stable polysubstituted pyrrolidine derivatives.     

Specific intramolecular aromatic CH insertion of diazosulfonamides

The chemoselectivity in the intramolecular CH insertion of various diazosulfonamides has been experimentally studied. The results reveal that the aliphatic 1,4-, 1,5-, or 1,6-C(sp³)?H insertions of diazosulfonamides are not accessible, while the aromatic 1,5-C(sp²)?H insertion can be realized specifically by adjusting the diazo-adjacent group. In addition, the general chemoselectivities in the intramolecular CH insertions of diazosulfonyl compounds are summarized. Generally, diazosulfones undergo both aromatic 1,5-C(sp²)?H and aliphatic 1,5- and 1,6-C(sp³)?H insertions, while diazosulfonates undergo aliphatic 1,5- and 1,6-C(sp³)?H insertions. However, diazosulfonamides only undergo aromatic 1,5-C(sp²)?H insertion.     

N-Heterocyclic carbene-palladacyclic complexes: synthesis,characterization and their applications in the C-N coupling and α-arylation of ketones using aryl chlorides

N-Heterocyclic carbene-palladacyclic complexes 3 were successfully achieved in a one-pot procedure under mild conditions. The structure of 3a was unambiguously confirmed by X-ray single crystal diffraction and it was an active catalyst in the Buchwald-Hartwig amination and α-arylation of ketones even at very low catalyst loadings (0.01?mol%).     

Iodine-mediated oxidative Pictet-Spengler reaction using terminal alkyne as the 2-oxoaldehyde surrogate for the synthesis of 1-aroyl-β-carbolines and fused-nitrogen heterocycles

An efficient iodine-mediated oxidative Pictet-Spengler reaction in dimethyl sulphoxide (DMSO) using terminal alkynes as the 2-oxoaldehyde surrogate for the synthesis of aryl (9H-pyrido[3,4-b]indol-1-yl)methanones is described. The scope of the protocol includes the total synthesis of Fascaplysin, Eudistomins Y₁ and Y₂. The methodology is extended for preparing pyrrolo[1,2-a]-quinoxaline and indolo[1,5-a]quinoxaline derivatives. The utility of 1-aroyl-β-carbolines was demonstrated by performing palladium-catalyzed β-carboline directed ortho-C(sp2)-H functionalization of the phenyl ring with thiomethyl (SMe) group using DMSO as source and for accessing 4-aryl-canthin-6-ones.     

Facile synthesis of bicyclic 1-arylpyrazol-5-ones

In this Letter, we described a facile method for constructing fused bicyclic 1-arylpyrazol-5-one ring system. We employed various methylene-containing carboxylic acids as the substrates and proved that the pyrazolone ring closure requires activated methylene group in intermediate II. Accordingly, a series of structurally diversified, fused bicyclic 1-arylpyrazol-5-ones was prepared in moderate to high yields using the requisite substrates.     

A carbanion induced synthesis of highly congested pyrazole and imidazole containing heterocycles

An efficient approach to the synthesis of highly congested di, penta and hexacyclic pyrazoles as well as imidazole fragment containing novel heterocyclic molecule has been developed through a carbanion induced transformation of suitably functionalized 2H-pyran-2-ones, benzo[h]chromene and thiochromeno[4,3-b]pyrans. Due to the presence of fluorescence, we report their prime application metal sensor as off/on switching in ferric ions.     

Synthesis of pyrrolo[1,2-a]pyrazines and pyrazino[1,2-a]indoles by Curtius reaction in Morita-Baylis-Hillman derivatives

Synthesis of substituted pyrrolo[1,2-a]pyrazines and pyrazino[1,2-a]indoles from the Morita-Baylis-Hillman derivatives of acrylates via saponification followed by Curtius reaction is described.     

Selective synthesis of 4,5-dihydroimidazo- and imidazo[1,5-a]quinoxalines via modified Pictet–Spengler reaction

An efficient tandem approach for the selective synthesis of 4,5-dihydroimidazo[1,5-a]quinoxalines 6a–g and imidazo[1,5-a]quinoxalines 7a–h by the reaction of 2-imidazolyl anilines 4a–c with aryl aldehydes 5a–k under mild reaction conditions is described. Introduction of electron releasing alkyl groups in substrates 4a–b was found to be instrumental for the success of the reaction.     

Understanding the Diels-Alder reactivity of 1,2-azaborine analogues

The Diels-Alder reactivity of 1,2-heteroborines (H₄C₄B(H)X, X?=?NH, PH, AsH; O, S, Se) has been computationally explored by means of Density Functional Theory (DFT) calculations. The influence of the HB?=?X fragment on the reactivity of the system has been quantitatively analyzed in detail by means of the so-called Activation Strain Model (ASM) of reactivity. It is found that the interaction between these species and the dienophile is significantly stronger than that computed for their all-carbon isoelectronic counterpart, benzene. In addition, the strain energy plays a key role in the observed reactivity trends. The role of the aromaticity strength of these heteroarenes on the reactivity is also assessed.     

Synthesis of N-substituted carbazolones from α-iodo enaminones via Pd(0)-catalyzed intramolecular coupling under microwave irradiation

A variety of N-aryl and N-alkyl carbazolones were conveniently achieved in good to high yields via Pd₂(dba)₃-mediated intramolecular coupling of N-substituted α-iodo enaminones under microwave irradiation. The Pd(0)-catalyzed cyclization was found to proceed favorably with the more electron-deficient phenyl ring during the reactions involving unsymmetrical N,N-diaryl α-iodo enaminones. This unique property enables the construction of carbazolone skeleton containing nitro substituted benzenoid ring.